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- Title
Synthesis and Evaluation of N-Labelled Azo Compounds for β-Amyloid Imaging in Mice.
- Authors
Gaja, Vijay; Gómez-Vallejo, Vanessa; Puigivila, Maria; Pérez-Campaña, Carlos; Martin, Abraham; García-Osta, Ana; Calvo-Fernández, Teresa; Cuadrado-Tejedor, Mar; Franco, Rafael; Llop, Jordi
- Abstract
Purpose: The aim of the present study was to develop short half-lived tools for in vitro and in vivo β-amyloid imaging in mice, for which no suitable PET tracers are available. Procedures: Five N-labelled azo compounds ( 1- 5) were synthesized using a three-step process using cyclotron-produced [N]NO. Biodistribution studies were performed using positron emission tomography-computed tomography (PET-CT) on 20-month-old healthy, wild-type (WT) mice. In vivo and in vitro binding assays were performed using PET-CT and autoradiography, respectively, on 20-month-old healthy (WT) mice and transgenic (Tg2576) Alzheimer's disease model mice. Results: N-labelled azo compounds were prepared with decay corrected radiochemical yields in the range 27 ± 4 % to 39 ± 4 %. Biodistribution studies showed good blood-brain barrier penetration for compounds 1 and 3-5; good clearance data were also obtained for compounds 1-3 and 5. Compounds 2, 3 and 5 (but not 1) showed a significant uptake in β-amyloid-rich structures when assayed in in vitro autoradiographic studies. PET studies showed significant uptake of compounds 2 and 3 in the cortex of transgenic animals that exhibit β-amyloid deposits. Conclusions: The results underscore the potential of compounds 2 and 3 as in vitro and in vivo markers for β-amyloid in animal models of Alzheimer's disease.
- Subjects
AMYLOID; AZO compound synthesis; POSITRON emission tomography; AUTORADIOGRAPHY; LABORATORY mice; IN vitro studies
- Publication
Molecular Imaging & Biology, 2014, Vol 16, Issue 4, p538
- ISSN
1536-1632
- Publication type
Article
- DOI
10.1007/s11307-013-0708-x